The farnesoid X receptor (FXR) as a new target in non-alcoholic steatohepatitis
The farnesoid X receptor (FXR) as a new target in non-alcoholic steatohepatitis
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DOI：
10.1016/s1262-3636(08)74605-6
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发表时间：
2008-12-01
影响因子：
7.2
通讯作者：
Cariou, B.
中科院分区：
文献类型：
--
作者：
Cariou, B.
法尼醇X受体（FXR）是核受体超家族的成员，主要表达于肝、肠、肾和脂肪组织中。被胆汁酸激活后，FXR 调节多种靶基因，这些基因与胆汁酸、脂质和葡萄糖稳态的控制密切相关。因此，FXR 似乎是治疗非酒精性脂肪性肝炎 (NASH) 的有希望的靶点。值得注意的是，FXR 激活可抑制肝脏从头脂肪生成，增加胰岛素敏感性并保护肝细胞免受胆汁酸引起的细胞毒性。最近的数据还表明 FXR 在肝再生和肝癌发生中发挥着关键作用。因此，FXR 激动剂和/或调节剂 (SBARM) 的开发可能被证明在临床上可用于治疗 NASH。虽然啮齿类动物的临床前研究支持这一假设，但人类的临床研究仍然有必要。 (C) 2008 Elsevier Masson SAS。版权所有。
The farnesoid X receptor (FXR) is a member of the nuclear receptor superfamily that is mainly expressed in liver, intestine, kidney and adipose tissue. On activation by bile acids, FXR regulates a wide variety of target genes that are critically involved in the control of bile acid, lipid and glucose homeostasis. Thus, FXR appears to be a promising target for the treatment of non-alcoholic steatohepatitis (NASH). Notably, FXR activation inhibits hepatic de novo lipogenesis, increases insulin sensitivity and protects hepatocytes against bile acid-incluced cytotoxicity. More recent data also indicate a critical role of FXR in liver regeneration and hepatocarcinogenesis. For this reason, the development of FXR agonists and/or modulators (SBARMs) may prove to be clinically useful for treating NASH. While preclinical Studies in rodents Support this hypothesis, clinical studies are still warranted in humans. (C) 2008 Elsevier Masson SAS. All rights reserved.